A very serious problem in modern medicine, veterinary medicine and plant cultivation is treatment of fungal, bacterial and viral diseases, many of which respond to therapy very poorly. This is due to lack of efficiency of existing drugs and variability of bacteria, leading to the emergence of resistant forms (see Fidel P. L. Jr, Vazquez J. A., Sobel J. D. Candida glabrata: review of epidemiology, pathogenesis and clinical disease with comparison to C. albicans 1999, 1:80-96. White T. Antifungal drug resistance in Candida albicans ASM News 8:427-433.
The above is important for veterinary medicine and industry, because there is deterioration of products due to development and spread of microorganisms.
There is a number of drugs for treatment of fungal infections: nystatin, amphotericin B, fluconazole and terbinafine (RLS medications Encyclopedia—2009, RLS, 2009. Moscow, 928). Each of them has significant drawbacks. Fluconazole exhibits mainly fungistatic effect and practically does not possess fungicidal properties [Pharmaceutical microbiology. Ed. by W. B. Hugo and A. D. Rassel Blackwell Scientific Publications, Oxford, 1987, 511 p].
Fluconazole may also be used to prevent deterioration of plants and agricultural products by fungi. It is also known that fluconazole is used in archive-keeping for paper treatment.
The main drawback of Nystatin is the low activity against multicellular fungi.
Amphotericin B is an active antifungal preparation, but it is very toxic.
There is a fungicidal agent, which is notable for the fact that it is a salt of 2,4-dioxo-5-(2-hydroxy-3,5-dichlorobenzylidene)amino-1,3-pyrimidine:
or its dimer:
wherein X is selected from the series: Na+, K+, Li+, NH4+, RU 2448960 Cl.
This technical solution is taken as a prototype of the present invention.
The drug has a pronounced antifungal activity with wide spectrum of effect.
However, this compound is very poorly soluble in aqueous media and in fats. The maximum value of solubility of the known drug in water is 0.002%, and for fats it is no more than 0.001% (octanol, which is a common model of lipids). The low solubility of the fungicidal agent prototype is due to the fact that the substance has a large particle size: length—30 mkm and section—about 300 nm, which does not promote dissolution of the substance neither in an aqueous medium nor in fats. Solutions with such concentration of the active substance are not sufficiently effective. At the same time the task of improvement of efficiency of use of a fungicidal agent in the form of solutions for use in human and veterinary medicine in the form of injections and inhalations and for treatment of a variety of materials and agricultural products is extremely urgent.